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探讨外用药物生物利用度及生物等效性的函数确定方法及影响因素,并介绍一种定量的物理模型。该模型的假定条件是:①靶位置在表皮深部(基底层)及真皮;②在靶位置热力活性(即游离的活性药物浓度C~*)与药效相关。应用该模型要首先以实验测出的输入参数(角层、活性表皮及真皮的分配系数K,稳态透过系数P)证实有限量药物在皮肤中摄取/转运的三级模式。氢化可的松为模型药,无毛豚鼠的皮肤为模型膜,本模型通过概念C~*旨在表明配方因素如何影响生物利用度及生物等效性。最后,介绍应用合适的体外资料及物理模型计算预测外用配方的疗效。
To explore the methods and influencing factors of bioavailability and bioequivalence of topical drugs, and to introduce a quantitative physical model. The model assumes that: â ’target location in the deep epidermis (basal layer) and the dermis; â’ thermal activity at the target location (ie free active drug concentration C ~ *) and efficacy. The application of this model first confirms the tertiary modes of uptake / transport of a limited number of drugs in the skin with experimentally measured input parameters (distribution coefficient K of the cornea, active epidermis and dermis, and steady-state transmissivity P). Hydrocortisone is used as a model drug, and hairless guinea pig skin is used as a model membrane. This model, through the concept C *, is intended to show how formulation factors affect bioavailability and bioequivalence. Finally, the application of appropriate in vitro data and physical models to predict the efficacy of topical formulations is described.